Title:
溶融三環系スルホンアミドγセクレターゼ阻害剤
Document Type and Number:
Japanese Patent JP2009539773
Kind Code:
A
Abstract:
The invention provides compounds of formula I:
or pharmaceutically salts thereof, where R 1 , R 2 and the A, B, and C-rings are as defined herein. Compounds of formula I are useful in treating or preventing cognitive disorders, such as Alzheimer's disease. The invention also encompasses pharmaceutical compositions comprising compounds or salts of formula I, methods of preparing the desired compunds, and methods of treating cognitive disorders, such as Alzheimer's disease, using the compounds or salts of formula I.
Inventors:
Conrady, Andrey, W.
Probst, Gary
Aubele, Daniel, Elle.
Garofalo, Albert, W.
Homme, Roy
Nightsell, Martin, Elle.
Semco, Christopher, M.
Chuon, Anne, Pee.
Probst, Gary
Aubele, Daniel, Elle.
Garofalo, Albert, W.
Homme, Roy
Nightsell, Martin, Elle.
Semco, Christopher, M.
Chuon, Anne, Pee.
Application Number:
JP2009513467A
Publication Date:
November 19, 2009
Filing Date:
June 01, 2007
Export Citation:
Assignee:
PHARMACIA & UPJOHN COMPANY
International Classes:
C07D215/22; A61K31/437; A61K31/4375; A61K31/47; A61K31/4745; A61K31/519; A61P1/04; A61P1/16; A61P3/04; A61P3/10; A61P5/14; A61P7/10; A61P9/10; A61P9/12; A61P9/14; A61P11/02; A61P11/06; A61P11/16; A61P13/12; A61P15/00; A61P17/00; A61P17/02; A61P17/06; A61P17/12; A61P17/14; A61P19/02; A61P19/04; A61P19/08; A61P25/00; A61P25/28; A61P27/02; A61P29/00; A61P31/18; A61P35/00; A61P35/02; A61P35/04; A61P41/00; A61P43/00; C07D471/04; C07D471/14; C07D487/14; C07D495/14; C07D513/14
Domestic Patent References:
| JPH0977752A | 1997-03-25 | |||
| JP2001518469A | 2001-10-16 |
Foreign References:
| WO2004058772A1 | 2004-07-15 | |||
| WO2003024936A1 | 2003-03-27 | |||
| WO2005113542A2 | 2005-12-01 |
Other References:
JPN5009007871; ＢＡＲＵＮ Ｏ: ＴＥＴＲＡＨＥＤＲＯＮ ＬＥＴＴＥＲＳ Ｖｏｌ．４０， Ｎｏ．１１９, 19990507, ｐ．３７９７-３８００, ＥＬＳＥＶＩＥＲ
JPN5009007872; ＭＡＪＵＭＤＡＲ Ｓ: ＴＥＴＲＡＨＥＤＲＯＮ ＬＥＴＴＥＲＳ Ｖｏｌ．３８， Ｎｏ．４９, 19971208, ｐ．８５８１-４, ＥＬＳＥＶＩＥＲ
JPN5009007874; ＳＡＮＧＷＡＮ Ｎ Ｋ: ＩＮＤＩＡＮ ＪＯＵＲＮＡＬ ＯＦ ＣＨＥＭＩＳＴＲＹ，ＳＥＣＴＩＯＮ Ｂ Ｖ２４Ｂ, 198506, Ｐ６３９-６４４, ＰＵＢＬＩＣＡＴＩＯＮＳ ＆ ＩＮＦＯＲＭＡＴＩＯＮＳ ＤＩＲＥＣＴＯＲＡＴＥ
JPN6012053445; ＭＯＲＩＷＡＫＥ，Ｔ． ｅｔ ａｌ: 'Ｈｅｔｅｒｏｃｙｃｌｅｓ． ＩＩＩ． Ｓｙｎｔｈｅｓｅｓ ｏｆ Ｎ-ｔｏｓｙｌ-３-ｃａｒｂｏｍｅｔｈｏｘｙ-３-ｍｅｔｈｙｌ-４-ｏｘｏ- １，２，３，４-ｔｅｔｒａｈｙｄｒｏｑｕｉｎｏｌｉｎｅ' Ｊｏｕｒｎａｌ ｏｆ Ｍｅｄｉｃｉｎａｌ Ｃｈｅｍｉｓｔｒｙ Ｖｏｌ．１１， Ｎｏ．３, 1968, ｐ．６３６-７
JPN5009007873; ＫＥＬＫＡＲ Ｐ Ｍ: Ｉｎｄｉａｎ Ｊｏｕｒｎａｌ ｏｆ Ｃｈｅｍｉｓｔｒｙ， Ｓｅｃｔｉｏｎ Ｂ Ｖｏｌ．１９Ｂ， Ｎｏ．４, 198004, ｐ．２９７-３００, ＰＵＢＬＩＣＡＴＩＯＮＳ ＆ ＩＮＦＯＲＭＡＴＩＯＮＳ ＤＩＲＥＣＴＯＲＡＴＥ
JPN6012053441; ＳＡＮＧＷＡＮ，Ｎ．Ｋ． ｅｔ ａｌ: 'Ｓｔｕｄｉｅｓ ｉｎ ａｎｔｉｆｅｒｔｉｌｉｔｙ ａｇｅｎｔｓ． Ｐａｒｔ ＸＸＸＩＩ． Ｓｙｎｔｈｅｓｉｓ ａｎｄ ｓｔｅｒｅｏｃｈｅｍｉｓｔｒｙ ｏｆ ３，３ａ-ｔｒａｎｓ- ａｎｄ ｃｉｓ-' Ｉｎｄｉａｎ Ｊｏｕｒｎａｌ ｏｆ Ｃｈｅｍｉｓｔｒｙ， Ｓｅｃｔｉｏｎ Ｂ： Ｏｒｇａｎｉｃ Ｃｈｅｍｉｓｔｒｙ Ｉｎｃｌｕｄｉｎｇ Ｍｅｄｉｃｉｎａｌ Ｃｈｅｍｉｓｔｒｙ Ｖｏｌ．２０Ｂ， Ｎｏ．２, 1981, ｐ．１３５-９
JPN6012053442; ＫＵＭＡＲ，Ａ． ｅｔ ａｌ: 'Ｋｅｔｅｎｅ ｄｉｔｈｉｏａｃｅｔａｌｓ． Ｐａｒｔ １２． Ｓｙｎｔｈｅｓｉｓ ａｎｄ ｒｅａｃｔｉｏｎｓ ｏｆ alpha-ｏｘｏｋｅｔｅｎｅ ｄｉｔｈｉｏａｃｅｔａｌｓ ｄｅｒｉｖｅｄ ｆｒｏｍ ｈｅ' Ｊｏｕｒｎａｌ ｏｆ Ｃｈｅｍｉｃａｌ Ｒｅｓｅａｒｃｈ， Ｓｙｎｏｐｓｅｓ Ｎｏ．８, 1979, ｐ．２６８-９
JPN6012053443; ＭＯＲＩＷＡＫＥ，Ｔ． ｅｔ ａｌ: 'Ｈｅｔｅｒｏｃｙｃｌｅｓ． ４． Ｓｙｎｔｈｅｓｅｓ ｏｆ ｂｅｎｚｏ［ｈ］ ｑｕｉｎｏｌｉｎｅ ｄｅｒｉｖａｔｉｖｅｓ' Ｊｏｕｒｎａｌ ｏｆ Ｍｅｄｉｃｉｎａｌ Ｃｈｅｍｉｓｔｒｙ Ｖｏｌ．１４， Ｎｏ．１, 1971, ｐ．８５
JPN6012053444; ＳＰＥＣＫＡＭＰ，Ｗ．Ｎ． ｅｔ ａｌ: 'Ｄｉｈｙｄｒｏｑｕｉｎｏｌｏｎｅｓ． Ｖ． Ｈｉｎｄｅｒｅｄ ｉｎｖｅｒｓｉｏｎ ｉｎ ｄｉｈｙｄｒｏｑｕｉｎｏｌｏｎｅｓ ａｎｄ ｒｅｌａｔｅｄ ｓｙｓｔｅｍｓ' Ｔｅｔｒａｈｅｄｒｏｎ Ｖｏｌ．２２， Ｎｏ．８, 1966, ｐ．２４１３-２７
JPN5009007872; ＭＡＪＵＭＤＡＲ Ｓ: ＴＥＴＲＡＨＥＤＲＯＮ ＬＥＴＴＥＲＳ Ｖｏｌ．３８， Ｎｏ．４９, 19971208, ｐ．８５８１-４, ＥＬＳＥＶＩＥＲ
JPN5009007874; ＳＡＮＧＷＡＮ Ｎ Ｋ: ＩＮＤＩＡＮ ＪＯＵＲＮＡＬ ＯＦ ＣＨＥＭＩＳＴＲＹ，ＳＥＣＴＩＯＮ Ｂ Ｖ２４Ｂ, 198506, Ｐ６３９-６４４, ＰＵＢＬＩＣＡＴＩＯＮＳ ＆ ＩＮＦＯＲＭＡＴＩＯＮＳ ＤＩＲＥＣＴＯＲＡＴＥ
JPN6012053445; ＭＯＲＩＷＡＫＥ，Ｔ． ｅｔ ａｌ: 'Ｈｅｔｅｒｏｃｙｃｌｅｓ． ＩＩＩ． Ｓｙｎｔｈｅｓｅｓ ｏｆ Ｎ-ｔｏｓｙｌ-３-ｃａｒｂｏｍｅｔｈｏｘｙ-３-ｍｅｔｈｙｌ-４-ｏｘｏ- １，２，３，４-ｔｅｔｒａｈｙｄｒｏｑｕｉｎｏｌｉｎｅ' Ｊｏｕｒｎａｌ ｏｆ Ｍｅｄｉｃｉｎａｌ Ｃｈｅｍｉｓｔｒｙ Ｖｏｌ．１１， Ｎｏ．３, 1968, ｐ．６３６-７
JPN5009007873; ＫＥＬＫＡＲ Ｐ Ｍ: Ｉｎｄｉａｎ Ｊｏｕｒｎａｌ ｏｆ Ｃｈｅｍｉｓｔｒｙ， Ｓｅｃｔｉｏｎ Ｂ Ｖｏｌ．１９Ｂ， Ｎｏ．４, 198004, ｐ．２９７-３００, ＰＵＢＬＩＣＡＴＩＯＮＳ ＆ ＩＮＦＯＲＭＡＴＩＯＮＳ ＤＩＲＥＣＴＯＲＡＴＥ
JPN6012053441; ＳＡＮＧＷＡＮ，Ｎ．Ｋ． ｅｔ ａｌ: 'Ｓｔｕｄｉｅｓ ｉｎ ａｎｔｉｆｅｒｔｉｌｉｔｙ ａｇｅｎｔｓ． Ｐａｒｔ ＸＸＸＩＩ． Ｓｙｎｔｈｅｓｉｓ ａｎｄ ｓｔｅｒｅｏｃｈｅｍｉｓｔｒｙ ｏｆ ３，３ａ-ｔｒａｎｓ- ａｎｄ ｃｉｓ-' Ｉｎｄｉａｎ Ｊｏｕｒｎａｌ ｏｆ Ｃｈｅｍｉｓｔｒｙ， Ｓｅｃｔｉｏｎ Ｂ： Ｏｒｇａｎｉｃ Ｃｈｅｍｉｓｔｒｙ Ｉｎｃｌｕｄｉｎｇ Ｍｅｄｉｃｉｎａｌ Ｃｈｅｍｉｓｔｒｙ Ｖｏｌ．２０Ｂ， Ｎｏ．２, 1981, ｐ．１３５-９
JPN6012053442; ＫＵＭＡＲ，Ａ． ｅｔ ａｌ: 'Ｋｅｔｅｎｅ ｄｉｔｈｉｏａｃｅｔａｌｓ． Ｐａｒｔ １２． Ｓｙｎｔｈｅｓｉｓ ａｎｄ ｒｅａｃｔｉｏｎｓ ｏｆ alpha-ｏｘｏｋｅｔｅｎｅ ｄｉｔｈｉｏａｃｅｔａｌｓ ｄｅｒｉｖｅｄ ｆｒｏｍ ｈｅ' Ｊｏｕｒｎａｌ ｏｆ Ｃｈｅｍｉｃａｌ Ｒｅｓｅａｒｃｈ， Ｓｙｎｏｐｓｅｓ Ｎｏ．８, 1979, ｐ．２６８-９
JPN6012053443; ＭＯＲＩＷＡＫＥ，Ｔ． ｅｔ ａｌ: 'Ｈｅｔｅｒｏｃｙｃｌｅｓ． ４． Ｓｙｎｔｈｅｓｅｓ ｏｆ ｂｅｎｚｏ［ｈ］ ｑｕｉｎｏｌｉｎｅ ｄｅｒｉｖａｔｉｖｅｓ' Ｊｏｕｒｎａｌ ｏｆ Ｍｅｄｉｃｉｎａｌ Ｃｈｅｍｉｓｔｒｙ Ｖｏｌ．１４， Ｎｏ．１, 1971, ｐ．８５
JPN6012053444; ＳＰＥＣＫＡＭＰ，Ｗ．Ｎ． ｅｔ ａｌ: 'Ｄｉｈｙｄｒｏｑｕｉｎｏｌｏｎｅｓ． Ｖ． Ｈｉｎｄｅｒｅｄ ｉｎｖｅｒｓｉｏｎ ｉｎ ｄｉｈｙｄｒｏｑｕｉｎｏｌｏｎｅｓ ａｎｄ ｒｅｌａｔｅｄ ｓｙｓｔｅｍｓ' Ｔｅｔｒａｈｅｄｒｏｎ Ｖｏｌ．２２， Ｎｏ．８, 1966, ｐ．２４１３-２７
Attorney, Agent or Firm:
Asamura patent office
Hideto Asamura
Hajime Asamura
Yukihiro Ikeda
Naganuma Akio
Kajiwara Saiko
Shinmura Morio
Kanamori Koji
Yuko Nagase
Youichi Inoue
Hideto Asamura
Hajime Asamura
Yukihiro Ikeda
Naganuma Akio
Kajiwara Saiko
Shinmura Morio
Kanamori Koji
Yuko Nagase
Youichi Inoue